Appearance Properties
It appears as a white crystalline powder at room temperature, hygroscopic, easily soluble in water, heated while dissolving.
Fosfomycin Sodium can combine with a bacterial cell wall synthesis enzyme, hinder bacterial cell wall synthesis related substances utilizing at the first reaction, which in turn has a bactericidal effect. have antibacterial effect for Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli, Neisseria gonorrhoeae, Proteus mirabilis, Salmonella typhi, Serratia bacteria, most Pseudomonas aeruginosa, Streptococcus pyogenes, Streptococcus faecalis, part indole-positive Proteus and certain Klebsiella, Enterobacter bacteria. The main clinical applications of Fosfomycin Sodium include: urinary tract treatment of sensitive Gram-negative bacteria caused urinary system, infection of skin and soft tissue, respiratory, intestinal and other parts. It can also be combined with other antibiotics, the treatment of severe infections caused by susceptible strains such as sepsis, pulmonary, meningeal infections, peritonitis, adnexitis, intrauterine infections, pelvic inflammatory disease, osteomyelitis. Also in combination with vancomycin for the treatment of methicillin-resistant Staphylococcus aureus (MRSA) infection.
Pharmacological effects
1. Broad spectrum antibiotic, high bioavailability, rapid absorption, strong anti-bacterial, not diet affected. Fosfomycin Sodium displays effects on killing Gram-positive and Gram-negative bacteria, especially Pseudomonas aeruginosa, Proteus, Salmonella, and exhibit excellent antibacterial activity for a variety of drug-resistant Staphylococcus aureus and Escherichia coli. For usage in animals, there is no drug resistance and cross-resistance. Clinical effect is good.
2. Rapid sterilization: This product is a rapid fungicide, its role is still evident after 1-2 hours. About 25% of the E. coli were killed at 1 hour after exposured to Fosfomycin Sodium (12.5μg/ml), and all died within 4-6 hours. Pseudomonas aeruginosa and Staphylococcus aureus were also all killed at 4 and 8 hours.
3. Low toxicity, little irritation on the body, no acute toxicity and adverse reactions, no increased burden on the kidney.
4. Low residue: the eliminate time for the muscles and organs to reach the residual standard is 48-72 hours.
The above information is edited by the Chemicalbook of Tian Ye.
Indications
Mainly used for Staphylococcus aureus, streptococcus, E. coli, Salmonella and other gram-negative bacteria caused acute and chronic bowel disease treatment in chickens, ducks, pigs.
Usage and dosage
Used in water for livestock and poultry: every 100kg of water added the product 5-10 grams, 2 times a day, once every three days. Used in animal spices: 10-15 g of the product added to per 100kg feed, 2 times a day, once every three days.
Combination therapy
For the treatment of intestinal infections, Fosfomycin Sodium can combine with β-lactam, aminoglycoside.
For the treatment of respiratory and lung infections, combining with macrolides, β-lactam.
For staph infections, better combined with erythromycin, rifampin.
For the treatment of acute respiratory infections, sepsis, peritonitis ect., increase the dose. Need to combine with β-lactams or aminoglycosides.
Detection Indicator
No. Test item Export standard CP2000 Edition
1 Traits: A white crystalline powder, odorless, taste salty white crystalline powder, odorless, salty taste
2 Discriminator: Positive reaction Positive reaction
3 Specific rotation °-4.2 ~-5.5-4.2 ~-5.5
4 Heavy Metal ≤0.0010% 0≤.0010%
5 Content ≥700μ/mg ≥700μ/mg
6 Alkalinity 9.0-10.5 9.0-10.5
7 Weight loss on drying ≤1.0% ≤1.5% (water)
8 Solution clarity ≤No. 3/4 turbidity standards solution ≤No. 1 turbidity standard solution
9 Color of the solution ≤Yellow No. 1 ≤ Yellow No. 1
10 Glycols ≤0.50% ≤0.50%
11 Clarity of solution: can not be detected, in compliance with (a gross point ≤8/g, wherein a color point ≤2/g)
12 W ≤0.002%-
13 phosphorus content-16.2-17.9%
14 Sterile: Subject to compliance
15 Heat source/ bacterial endotoxin: compliance (heat source) compliance (bacterial endotoxin)
16 α-phenylethylamine ≤0.01%-
17 Residual amount of methanol: real
18 Residual amount of ethanol: Real
The above information is the main export detection index of fosfomycin.
Precautions
1. This product is mainly used for pigs, chickens, fish; application for other animals should medication under veterinary guidance.
2. Fosfomycin Sodiumand β-lactams, aminoglycosides, macrocyclic acid esters have a synergistic effect of combination therapy, and can reduce or delay the occurrence of bacterial resistance.
Uses
For the treatment of infections caused by Staphylococcus aureus, Escherichia coli, Proteus and Shigella.
Chemical Properties
White Solid
Uses
Disodium phosphonomycin, also known as Fosfomycin, is an antibiotic produced by Streptomyces fradiae. It is used to treat uncomplicated urinary tract infections and to reduce nephrotoxicity and ototoxicity of platinum-containing anti-tumor agents. It is used for susceptibility studies of Klebsiella pneumoniae and to study in vitro susceptibility testing procedures for fosfomycin tromethamine
Uses
Prevents peptidoglycan synthesis by inhibiting MurA, an enzyme responsible for synthesizing N-acetylmuramic acid or NAM, a major component of peptidoglycan
Uses
Curariform muscle relaxants
Biological Activity
Antibiotic th at concentrates in kidney and bladder; reduces nephrotoxicity and ototoxicity of platinum-containing anti-tumor agents. Fosfomycin is a phosphoenolpyruvate analog th at irreversibly inhibits UDP-GlcNAc enolpyruvyl tranferase (MurA), an enzyme involved in bacterial cell wall biosynthesis. As a result, the production of N-acetylmuramic acid, an essential element of the peptidoglycan cell wall, is inhibited.
in vivo
Fosfomycin sodium (80 mg/kg; i.v.-i.v. or i.v.-p.o.) displays the protective effect on the nephrotoxicity of double beckacin, and is not affected by different administration routes[3].
Pharmacokinetic of Fosfomycin sodium in Rats[4]
| Dibekacin Dose (mg) | Vdss (l/kg) | β (min-1) | T1/2 (min) | Urinary recovery (%) |
| 30 | 0.261 | 0.0244 | 28.4 | 85 |
| Animal Model: | Fischer 344 rats[3] |
| Dosage: | 320 mg/kg |
| Administration: | Intramuscular injection, 5 schedules: 1 h, 0.5 h earlier than dibekacin, concomitantly, 0.5 h later and 1 h later; 11 days |
| Result: | Reduced polyuria, proteinuria, enzymes and cytosine caused by dibecacin (40 mg/kg), followed by the previous treatment.
|
| Animal Model: | Dehydrated Wistar rat with acute renal failure (8-week-old)[4] |
| Dosage: | 120 mg/kg |
| Administration: | Intravenous injection; once |
| Result: | Recovered the exclusion rate of rats basically to normal, and improved the nephrotoxicity parameters.
Protects proximal tubular lysosomes from aminoglycosides by inhibiting myeloid formation and protecting the integrity of lysosomal membrane of rats treated with double bekacin.
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